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Review

Selective Raf inhibition in cancer therapy

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Pages 1587-1609 | Published online: 18 Nov 2007

Keep up to date with the latest research on this topic with citation updates for this article.

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Zhiyong Xiao, Feng Liu, Junping Cheng, Ying Wang, Wenxia Zhou & Yongxiang Zhang. (2023) B-Raf inhibitor vemurafenib counteracts sulfur mustard-induced epidermal impairment through MAPK/ERK signaling. Drug and Chemical Toxicology 46:2, pages 226-235.
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Fabienne Saab, Sylvain Routier, Jean-Yves Mérour, Valérie Bénéteau & Françoise Schoentgen. (2010) Comparison of the efficiencies of two TR-FRET methods to detect in vitro natural and synthesized inhibitors of the Raf/MEK/ERK signaling pathway. International Journal of High Throughput Screening 1, pages 81-98.
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Elisabeth Livingstone, Lisa Zimmer, Sarah Piel & Dirk Schadendorf. (2010) PLX4032: does it keep its promise for metastatic melanoma treatment?. Expert Opinion on Investigational Drugs 19:11, pages 1439-1449.
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Angela M Liu, Michelle Z Xu, Jinfei Chen, Ronnie T Poon & John M Luk. (2010) Targeting YAP and Hippo signaling pathway in liver cancer. Expert Opinion on Therapeutic Targets 14:8, pages 855-868.
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James A McCubrey, Linda S Steelman, Steven L Abrams, William H Chappell, Suzanne Russo, Roger Ove, Michele Milella, Agostino Tafuri, Paolo Lunghi, Antonio Bonati, Franca Stivala, Ferdinando Nicoletti, Massimo Libra, Alberto M Martelli, Giuseppe Montalto & Melchiorre Cervello. (2009) Emerging Raf inhibitors. Expert Opinion on Emerging Drugs 14:4, pages 633-648.
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E. F. Choo, J. P. Driscoll, J. Feng, B. Liederer, E. Plise, N. Randolph, Y. Shin, S. Wong & Y. Ran. (2009) Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species. Xenobiotica 39:9, pages 700-709.
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Stephen J. Harwood, Christopher R. Smith, J. David Lawson & John M. Ketcham. (2023) Selected Approaches to Disrupting Protein–Protein Interactions within the MAPK/RAS Pathway. International Journal of Molecular Sciences 24:8, pages 7373.
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Rahim Ullah, Qing Yin, Aidan H. Snell & Lixin Wan. (2022) RAF-MEK-ERK pathway in cancer evolution and treatment. Seminars in Cancer Biology 85, pages 123-154.
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Chris Wilson & John P Murnane. (2022) High-throughput screen to identify compounds that prevent or target telomere loss in human cancer cells. NAR Cancer 4:4.
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Zhenlin Wang, Mengchen Yin, Peilin Chu & Meiqing Lou. (2019) STAT3 inhibitor sensitized KRAS-mutant lung cancers to RAF inhibitor by activating MEK/ERK signaling pathway. Aging 11:17, pages 7187-7196.
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Salem & Hansen. (2019) The Hippo Pathway in Prostate Cancer. Cells 8:4, pages 370.
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Sultana Mehbuba Hossain, Jayalaxmi Shetty, Kyi Kyi Tha & Ezharul Hoque Chowdhury. (2019) α-Ketoglutaric Acid-Modified Carbonate Apatite Enhances Cellular Uptake and Cytotoxicity of a Raf-Kinase Inhibitor in Breast Cancer Cells through Inhibition of MAPK and PI-3 Kinase Pathways. Biomedicines 7:1, pages 4.
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Hsiu-Yu Liu, Andrea Z. Tuckett, Myles Fennell, Ralph Garippa & Johannes L. Zakrzewski. (2018) Repurposing of the CDK inhibitor PHA-767491 as a NRF2 inhibitor drug candidate for cancer therapy via redox modulation. Investigational New Drugs 36:4, pages 590-600.
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Amir Noeparast, Erik Teugels, Philippe Giron, Gil Verschelden, Sylvia De Brakeleer, Lore Decoster & Jacques De Grève. (2016) Non-V600 BRAF mutations recurrently found in lung cancer predict sensitivity to the combination of Trametinib and Dabrafenib. Oncotarget 8:36, pages 60094-60108.
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R Mandal, S Becker & K Strebhardt. (2015) Stamping out RAF and MEK1/2 to inhibit the ERK1/2 pathway: an emerging threat to anticancer therapy. Oncogene 35:20, pages 2547-2561.
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Waqar Aman, Junghun Lee, Minjung Kim, Songyi Yang, Hoyong Jung & Jung-Mi Hah. (2016) Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation. Bioorganic & Medicinal Chemistry Letters 26:4, pages 1188-1192.
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Su An, Yang Yang, Richard Ward, Ying Liu, Xiao-Xi Guo & Tian-Rui Xu. (2015) Raf-interactome in tuning the complexity and diversity of Raf function. FEBS Journal 282:1, pages 32-53.
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J-X Li, J-M Feng, Y Wang, X-H Li, X-X Chen, Y Su, Y-Y Shen, Y Chen, B Xiong, C-H Yang, J Ding & Z-H Miao. (2014) The B-RafV600E inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury. Cell Death & Disease 5:6, pages e1278-e1278.
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Hala Bakr El-Nassan. (2014) Recent progress in the identification of BRAF inhibitors as anti-cancer agents. European Journal of Medicinal Chemistry 72, pages 170-205.
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Miao Ding, Erlong Zhang, Rong He & Xingyong Wang. (2013) Newly developed strategies for improving sensitivity to radiation by targeting signal pathways in cancer therapy. Cancer Science 104:11, pages 1401-1410.
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Miriam Molina-Arcas, David C. Hancock, Clare Sheridan, Madhu S. Kumar & Julian Downward. (2013) Coordinate Direct Input of Both KRAS and IGF1 Receptor to Activation of PI3 kinase in KRAS -Mutant Lung Cancer . Cancer Discovery 3:5, pages 548-563.
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Feng Jin, Dan Gao, Cunlong Zhang, Feng Liu, Bizhu Chu, Yan Chen, Yu Zong Chen, Chunyan Tan & Yuyang Jiang. (2013) Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors of Raf1 and JNK1 kinases for anti-tumor treatment. Bioorganic & Medicinal Chemistry 21:3, pages 824-831.
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Vipin Yadav, Xiaoyi Zhang, Jiangang Liu, Shawn Estrem, Shuyu Li, Xue-Qian Gong, Sean Buchanan, James R. Henry, James J. Starling & Sheng-Bin Peng. (2012) Reactivation of Mitogen-activated Protein Kinase (MAPK) Pathway by FGF Receptor 3 (FGFR3)/Ras Mediates Resistance to Vemurafenib in Human B-RAF V600E Mutant Melanoma. Journal of Biological Chemistry 287:33, pages 28087-28098.
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Do-Hee Kim & Taebo Sim. (2012) Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics. Archives of Pharmacal Research 35:4, pages 605-615.
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Chuan-Ming XU & Fu-Sheng WAN. (2012) Hippo signaling pathway in mammals:a new therapeutic target for tumors. Hereditas (Beijing) 34:3, pages 269-280.
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Hans-Peter Buchstaller, Lars Burgdorf, Dirk Finsinger, Frank Stieber, Christian Sirrenberg, Christiane Amendt, Matthias Grell, Frank Zenke & Mireille Krier. (2011) Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 21:8, pages 2264-2269.
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Li Ren, Steve Wenglowsky, Greg Miknis, Bryson Rast, Alex J. Buckmelter, Robert J. Ely, Stephen Schlachter, Ellen R. Laird, Nikole Randolph, Michele Callejo, Matthew Martinson, Sarah Galbraith, Barbara J. Brandhuber, Guy Vigers, Tony Morales, Walter C. Voegtli & Joseph Lyssikatos. (2011) Non-oxime inhibitors of B-RafV600E kinase. Bioorganic & Medicinal Chemistry Letters 21:4, pages 1243-1247.
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Armin Robubi, Herbert Waldmann  & Daniel Rauh. (2010) RAF Kinase Inhibitors in Cancer Treatment: Like a Bull in a China Shop?. ChemBioChem 11:12, pages 1645-1648.
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Martin McMahon. (2010) RAF translocations expand cancer targets. Nature Medicine 16:7, pages 749-750.
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Hana Yu, Yunkyung Jung, Hwan Kim, Junghun Lee, Chang-Hyun Oh, Kyung Ho Yoo, Taebo Sim & Jung-Mi Hah. (2010) 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 20:12, pages 3805-3808.
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Marco H. Hofmann, Jochen Heinrich, Gerald Radziwil & Karin Moelling. (2009) A Short Hairpin DNA Analogous to miR-125b Inhibits C-Raf Expression, Proliferation, and Survival of Breast Cancer Cells. Molecular Cancer Research 7:10, pages 1635-1644.
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Harvey Wong, Marcia Belvin, Sylvia Herter, Klaus P. Hoeflich, Lesley J. Murray, Leo Wong & Edna F. Choo. (2009) Pharmacodynamics of 2-{4-[(1 E )-1-(Hydroxyimino)-2,3-dihydro-1 H -inden-5-yl]-3-(pyridine-4-yl)-1 H -pyrazol-1-yl}ethan-1-ol (GDC-0879), a Potent and Selective B-Raf Kinase Inhibitor: Understanding Relationships between Systemic Concentrations, Phosphorylated Mitogen-Activated Protein Kinase Kinase 1 Inhibition, and Efficacy . Journal of Pharmacology and Experimental Therapeutics 329:1, pages 360-367.
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Joshua D. Hansen, Jonas Grina, Brad Newhouse, Mike Welch, George Topalov, Nicole Littman, Michele Callejo, Susan Gloor, Matthew Martinson, Ellen Laird, Barbara J. Brandhuber, Guy Vigers, Tony Morales, Rich Woessner, Nikole Randolph, Joseph Lyssikatos & Alan Olivero. (2008) Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorganic & Medicinal Chemistry Letters 18:16, pages 4692-4695.
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